公开(公告)号：US20200030260A1

公开(公告)日：2020-01-30

申请号：US16523568

申请日：2019-07-26

Applicant: Xenon Pharmaceuticals Inc.

Inventor： Robin Paul Sherrington ,  Jean-Jacques Alexandre Cadieux ,  Parisa Karimi Tari ,  Jeffrey Paul Bechard

IPC: A61K31/137 ,  A61K31/24 ,  A61P25/08

Abstract: In certain embodiments, the present disclosure is directed to methods and uses for treating a mammal having an epileptic seizure disorder or being at risk for having an epileptic seizure disorder, comprising administering certain herein disclosed isolated fenfluramine enantiomers that are surprisingly effective as anti-epilepsy drugs (AEDs), despite having lower anti-seizure potency than fenfluramine racemate, by virtue of also being less cardiotoxic than fenfluramine racemate. Preferred embodiments contemplate treatment of Dravet syndrome; other preferred embodiments contemplate treatment of other epileptic seizure disorders.

公开(公告)号：US20190031607A1

公开(公告)日：2019-01-31

申请号：US16150070

申请日：2018-10-02

Applicant: GENENTECH, INC. ,  XENON PHARMACEUTICALS INC.

Inventor： Jean-Christophe ANDREZ ,  Philippe BERGERON ,  Paul Robert BICHLER ,  Sultan CHOWDHURY ,  Christoph Martin DEHNHARDT ,  Thilo FOCKEN ,  Wei GONG ,  Michael Edward GRIMWOOD ,  Abid HASAN ,  Ivan William HEMEON ,  Qi JIA ,  Brian Salvatore SAFINA ,  Shaoyi SUN ,  Michael Scott WILSON ,  Alla Yurevna ZENOVA

IPC: C07D207/16 ,  C07C235/52 ,  C07D209/02 ,  C07D401/10 ,  C07D205/04 ,  C07D207/22 ,  C07D211/20 ,  C07C235/42 ,  C07D211/38 ,  C07D409/06 ,  C07D265/30 ,  C07D413/12 ,  C07D263/26 ,  C07C235/54 ,  C07D417/12 ,  C07D305/08 ,  C07D213/69 ,  C07D403/04 ,  C07D231/06 ,  C07D209/52 ,  C07D221/22 ,  C07D209/54 ,  C07D403/12 ,  C07D211/60 ,  C07D207/10 ,  C07D401/12 ,  C07D471/08 ,  C07D413/14 ,  C07D207/08 ,  C07D405/10 ,  C07D403/14 ,  C07D451/02 ,  C07D401/14 ,  C07D263/04 ,  C07D277/06

CPC classification number: C07D207/16 ,  C07C235/42 ,  C07C235/52 ,  C07C235/54 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2603/74 ,  C07D205/04 ,  C07D207/08 ,  C07D207/10 ,  C07D207/22 ,  C07D209/02 ,  C07D209/52 ,  C07D209/54 ,  C07D211/20 ,  C07D211/38 ,  C07D211/60 ,  C07D213/69 ,  C07D221/22 ,  C07D231/06 ,  C07D263/04 ,  C07D263/26 ,  C07D265/30 ,  C07D277/06 ,  C07D305/08 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/10 ,  C07D409/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D451/02 ,  C07D471/08

Abstract: The invention provides compounds having the general Formula (I); and pharmaceutically acceptable salts thereof; wherein the variables RA, RAA, subscript n, subscript q, ring A, X2, L, subscript m, X1, R1, R2, R3, R4, R5, D and E have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.

公开(公告)号：US20180346416A1

公开(公告)日：2018-12-06

申请号：US16057693

申请日：2018-08-07

Applicant: GENENTECH, INC. ,  XENON PHARMACEUTICALS INC.

Inventor： Christoph Martin DEHNHARDT ,  Sultan CHOWDHURY ,  Thilo FOCKEN ,  Michael Edward GRIMWOOD ,  Ivan William HEMEON ,  Brian Salvatore SAFINA ,  Daniel P. SUTHERLIN

IPC: C07C307/06 ,  C07D277/24 ,  C07D401/12 ,  C07D305/08 ,  C07D213/64 ,  C07D213/63 ,  C07D277/62 ,  C07D277/34 ,  C07D405/12 ,  C07D231/56 ,  C07D215/20 ,  C07D213/74 ,  C07D213/69 ,  C07D209/08 ,  C07D205/04 ,  C07D413/12 ,  C07D217/02

CPC classification number: C07C307/06 ,  C07C2601/04 ,  C07D205/04 ,  C07D209/08 ,  C07D213/63 ,  C07D213/64 ,  C07D213/69 ,  C07D213/74 ,  C07D215/20 ,  C07D217/02 ,  C07D231/56 ,  C07D277/24 ,  C07D277/34 ,  C07D277/62 ,  C07D305/08 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12

Abstract: The invention provides methods for treating pain using compounds having the general formula: and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, ring D, R1, and RN have the meaning as described herein.

公开(公告)号：US20180230079A1

公开(公告)日：2018-08-16

申请号：US15896970

申请日：2018-02-14

Applicant: GENENTECH, INC. ,  XENON PHARMACEUTICALS INC.

Inventor： Ivan William HEMEON ,  Brian SAFINA ,  Daniel SUTHERLIN

IPC: C07C62/38 ,  C07C62/34 ,  C07D211/22 ,  C07C323/61 ,  C07C317/44 ,  C07C313/04 ,  C07C229/48 ,  A61P17/04 ,  A61P25/00 ,  A61P29/00

CPC classification number: C07C62/38 ,  A61P17/04 ,  A61P25/00 ,  A61P29/00 ,  C07C62/34 ,  C07C69/757 ,  C07C229/48 ,  C07C313/04 ,  C07C317/44 ,  C07C323/61 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2603/74 ,  C07D211/22

Abstract: The invention provides compounds having the general formula I: and pharmaceutically acceptable salts thereof, wherein the variables RAA, n, ring A, X1, L, m, X2, R2, R3, R4, R5, X, and R6 have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.

公开(公告)号：US09546164B2

公开(公告)日：2017-01-17

申请号：US14603273

申请日：2015-01-22

Applicant: GENENTECH, INC. ,  XENON PHARMACEUTICALS INC.

Inventor： Jean-Christophe Andrez ,  Paul Robert Bichler ,  Chien-An Chen ,  Sultan Chowdhury ,  Shannon Marie Decker ,  Christoph Martin Dehnhardt ,  Thilo Focken ,  Michael Edward Grimwood ,  Ivan William Hemeon ,  Qi Jia ,  Jun Li ,  Zhiguo Liu ,  Daniel F. Ortwine ,  Brian Safina ,  Daniel Sutherlin ,  Tao Sheng ,  Shaoyi Sun ,  Andrew D. White ,  Michael Scott Wilson ,  Alla Yurevna Zenova ,  Jiuxiang Zhu

IPC: C07D211/32 ,  C07D211/54 ,  C07D233/68 ,  C07D453/02 ,  A61K31/337 ,  A61K31/397 ,  A61K31/4015 ,  A61K31/415 ,  A61K31/4412 ,  A61K31/495 ,  C07D237/08 ,  C07D241/04 ,  C07D205/04 ,  C07D207/12 ,  C07D211/42 ,  C07D305/08 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07D403/04 ,  C07D487/08 ,  C07D265/30 ,  C07D211/60

CPC classification number: A61K31/445 ,  A61K31/337 ,  A61K31/397 ,  A61K31/4015 ,  A61K31/415 ,  A61K31/4412 ,  A61K31/4523 ,  A61K31/4545 ,  A61K31/495 ,  C07D205/04 ,  C07D207/12 ,  C07D211/22 ,  C07D211/32 ,  C07D211/42 ,  C07D211/54 ,  C07D211/60 ,  C07D233/68 ,  C07D237/08 ,  C07D241/04 ,  C07D265/30 ,  C07D305/08 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D453/02 ,  C07D487/08 ,  C07F7/0812

Abstract: The invention provides compounds having the general formula I: and pharmaceutically acceptable salts thereof, wherein the variables RA, RAA, subscript n, ring A, X2, L, subscript m, X1, R1, R2, R3, R4, R5, and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.

Abstract translation: 本发明提供具有通式I的化合物及其药学上可接受的盐，其中变量RA，RAA，下标n，环A，X2，L，下标m，X1，R1，R2，R3，R4，R5和RN 具有本文所述的含义，以及含有这些化合物的组合物和使用这些化合物和组合物的方法。

公开(公告)号：US20160326184A1

公开(公告)日：2016-11-10

申请号：US14989600

申请日：2016-01-06

Applicant: XENON PHARMACEUTICALS INC.

Inventor： Jean-Jacques Alexandre Cadieux ,  Mikhail Chafeev ,  Sultan Chowdhury ,  Jianmin FU ,  Qi Jia ,  Stefanie Abel ,  Emad El-Sayed ,  Elke Huthmann ,  Thomas Isarno

IPC: C07D491/20 ,  C07D405/04

CPC classification number: C07D491/20 ,  C07D405/04

Abstract: This invention is directed to methods of preparing certain spiro-oxindole derivatives, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.

公开(公告)号：US09487535B2

公开(公告)日：2016-11-08

申请号：US13794147

申请日：2013-03-11

Applicant: Xenon Pharmaceuticals Inc.

Inventor： Shaoyi Sun ,  Jianmin Fu ,  Sultan Chowdhury ,  Ivan William Hemeon ,  Michael Edward Grimwood ,  Tarek Suhayl Mansour

IPC: C07D491/20 ,  C07D209/34 ,  C07D405/10 ,  C07D491/107

CPC classification number: C07D491/20 ,  C07D209/34 ,  C07D405/04 ,  C07D405/06 ,  C07D405/10 ,  C07D405/14 ,  C07D491/107

Abstract: This invention is directed to asymmetric syntheses of certain spiro-oxindole derivatives, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.

Abstract translation: 本发明涉及某些螺 - 羟吲哚衍生物的不对称合成，其可用于治疗和/或预防钠通道介导的疾病或病症如疼痛。

公开(公告)号：US09365578B2

公开(公告)日：2016-06-14

申请号：US14355549

申请日：2012-10-30

Applicant: XENON PHARMACEUTICALS INC.

Inventor： Shifeng Liu ,  Thilo Focken ,  Navjot Chahal ,  Zaihui Zhang ,  Renata Marcella Oballa ,  Julia Fonarev

IPC: C07D487/04 ,  C07D417/12 ,  C07D471/04 ,  C07D473/00 ,  C07D417/14 ,  C07D403/12

Abstract: This invention is directed to biaryl ether sulfonamides, or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.

公开(公告)号：US20150224071A1

公开(公告)日：2015-08-13

申请号：US14558440

申请日：2014-12-02

Applicant: GENENTECH, INC. ,  XENON PHARMACEUTICALS INC.

Inventor： Sultan Chowdhury ,  Christoph Martin Dehnhardt ,  Thilo Focken ,  Michael Edward Grimwood ,  Ivan William Hemeon ,  Qi Jia ,  Daniel Ortwine ,  Brian Safina ,  Shaoyi Sun ,  Daniel P. Sutherlin ,  Alla Yurevna Zenova

IPC: A61K31/18 ,  A61K31/397 ,  A61K31/40 ,  A61K31/5375 ,  A61K31/41 ,  A61K31/44 ,  A61K31/4164

CPC classification number: C07D491/107 ,  A61K31/18 ,  A61K31/397 ,  A61K31/40 ,  A61K31/41 ,  A61K31/4164 ,  A61K31/44 ,  A61K31/5375 ,  C07B2200/05 ,  C07C307/06 ,  C07C311/51 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2601/18 ,  C07C2602/10 ,  C07C2602/18 ,  C07C2602/20 ,  C07C2602/42 ,  C07C2602/44 ,  C07C2602/50 ,  C07C2603/66 ,  C07C2603/68 ,  C07C2603/74 ,  C07D205/04 ,  C07D207/46 ,  C07D207/48 ,  C07D209/52 ,  C07D211/22 ,  C07D211/96 ,  C07D213/64 ,  C07D213/82 ,  C07D233/84 ,  C07D257/04 ,  C07D265/30 ,  C07D295/192 ,  C07D295/26 ,  C07D307/12 ,  C07D307/18 ,  C07D309/08 ,  C07D311/58 ,  C07D311/70 ,  C07D311/72 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D451/02 ,  C07D471/08

Abstract: The invention provides novel compounds having the general formula: and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, B, R1, R2, R3, R4, R5 and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.

Abstract translation: 本发明提供具有以下通式的新化合物及其药学上可接受的盐，其中变量RA，下标n，环A，X2，L，下标m，X1，B，R1，R2，R3，R4，R5和RN具有 本文所述的含义，以及含有这些化合物的组合物和使用这些化合物和组合物的方法。

公开(公告)号：US20150025121A1

公开(公告)日：2015-01-22

申请号：US14510634

申请日：2014-10-09

Applicant: Xenon Pharmaceuticals Inc.

Inventor： Mikhail Chafeev ,  Jianmin Fu ,  Jean-Jacques Alexandre Cadieux

IPC: A61K31/407 ,  C07D491/20

CPC classification number: C07D491/20 ,  A61K31/407 ,  C07B57/00 ,  C07B2200/07 ,  C07D491/22

Abstract: This invention is directed to the (S)-enantiomer of the compound of formula (I): or a pharmaceutically acceptable solvate or prodrug thereof. This (S)-enantiomer is useful for the treatment of diseases or conditions, such as pain, which are ameliorated or alleviated by the modulation of voltage-gated sodium channels.

Abstract translation: 本发明涉及式（I）化合物的（S） - 对映异构体：或其药学上可接受的溶剂合物或前药。 该（S） - 对映体可用于治疗通过调节电压门控钠通道而改善或缓解的疾病或病症，例如疼痛。